21results about How to "Reduce systemic side effects" patented technology

The invention discloses an ROS-responsive prostate cancer targeting prodrug as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The prodrug is formed by covalently linking a prostate cancer targeting peptide SYEELR, a ROS (reactive oxygen species) response type ketal thiol (TK) connexon and an active molecule Devimistat. The preparation method comprises the following two steps: firstly, coupling Devimistat with a TK linker to obtain an intermediate Dev-TK, and then coupling the intermediate Dev-TK with an SYEELR peptide fragment to obtain a target product. The prodrug can specifically break and release Devimistat in a tumor high active oxygen microenvironment, and active targeting delivery is realized by virtue of the SYEELR peptide. The invention provides a novel prostatic cancer treatment strategy with accurate targeting, controllable release, enhanced curative effect and toxicity reduction potential.

The present application relates to the technical field of medical apparatus, particularly relates to wearable and vibration control nail base nanocrystal microneedle transdermal drug delivery device, including shell, both sides of the shell are provided with a group of positioning notches respectively, a group of positioning notches are provided with a threaded hole respectively, the inside four corners of the shell are provided with a group of support seats respectively, still include controller assembly, nanocrystal microneedle assembly, vibration assembly, power supply assembly and fixed ring assembly, the controller assembly is detachably installed in the shell, the shell is provided with vibration assembly and battery assembly respectively, the bottom end of the shell is detachably provided with nanocrystal microneedle assembly, the both ends of the fixed ring assembly are detachably connected with a group of positioning notches respectively, the nanocrystal microneedle assembly is used for lightly pricking nail base epidermis and nail plate edge to form microchannel, the power supply assembly provides power for vibration assembly and controller assembly;It makes drug directly contact focus.

The invention relates to the technical field of gouty arthritis, and discloses a traditional Chinese medicine plaster for treating gouty arthritis and a preparation method thereof. The ointment comprises the following materials: 1 part of paniculate swallowwort root, 1 part of asarum, 1 part of borneol, 2 parts of costustoot, 2 parts of earthworm, 3 parts of ligusticum wallichii, 3 parts of radix clematidis, 3 parts of spina gleditsiae, 4 parts of raw rhubarb, 6 parts of mint, a proper amount of vaseline, a proper amount of sesame oil, a medical dressing plaster and a desensitization adhesive tape. According to the traditional Chinese medicine plaster for treating the gouty arthritis and the preparation method of the traditional Chinese medicine plaster, the traditional Chinese medicine plaster directly acts on an affected part, transdermal absorption is achieved, the local treatment effect can be rapidly achieved, pains and inflammations caused by the gouty arthritis are relieved, medicinal materials are smashed into ultra-micro powder of 300 meshes through an ultra-micro powder machine, and the traditional Chinese medicine plaster is prepared into the traditional Chinese medicine plaster for treating the gouty arthritis. Compared with an oral medicine, the external plaster can increase the surface area of the medicine and improve the permeability and absorption efficiency of the medicine, and compared with the oral medicine, the external plaster can reduce the stimulation of the medicine to gastrointestinal tracts and systemic side effects.

The invention discloses a liver-targeting nitric oxide donor compound and application thereof. The compound is a derivative of 5-isosorbide mononitrate, and can be enriched in the liver and release nitric oxide. Compared with 5-isosorbide mononitrate, the compound disclosed by the invention is easier to metabolize after primary hepatocyte incubation of mice, effectively releases effector molecules such as nitric oxide and the like, shows good liver targeting, is expected to play a better effect in treatment of liver-related diseases, and improves the clinical application value of drugs.

The invention discloses an SPECT imaging device, an SPECT imaging system and a diagnosis combination. The SPECT imaging device comprises a rack and a nuclear detector group. The rack is provided with a through hole for a detected object to pass through. The through hole has a central axis. The nuclear detector group is arranged on the end face of the rack and comprises a plurality of longitudinal detectors arranged on the upper side and the lower side of the central axis and a plurality of transverse detectors arranged on the left side and the right side of the central axis, and the longitudinal detectors are used for obtaining longitudinal images of a detected object; the plurality of transverse detectors are used for acquiring a transverse image of the detected object, and the distance between the longitudinal detector and the central axis is smaller than that between the transverse detectors and the central axis. According to the SPECT imaging device, the collection efficiency is improved, the sensitivity is improved, and the resolution ratio of a detection image is improved.

This invention discloses a compound preparation for treating vascular dementia and its preparation method. The active pharmaceutical ingredient consists of protopanaxadiol and gallic acid in a 1:1 mass ratio, and the dosage form is liposomes. The preparation method includes extraction, mixing, liposome preparation, and optional freeze-drying steps: protopanaxadiol and gallic acid are extracted and purified from ginseng rhizome and Terminalia chebula fruit, respectively. After mixing, they are combined with phospholipids and cholesterol to prepare a lipid membrane. The membrane is then homogenized by hydration, low-temperature ultrasound, and high-pressure microfluidic jet to obtain a homogeneous liposome suspension, which can be further freeze-dried into a freeze-dried powder. The 1:1 composition of protopanaxadiol and gallic acid targets multiple points on the pathological mechanism of vascular dementia, showing significant therapeutic effects and broad application prospects. This preparation uses a liposome dosage form to improve the bioavailability of the active ingredient, the preparation process parameters are controllable, the active ingredient has high purity, the liposomes have uniform particle size, high encapsulation efficiency, and good stability.

The invention discloses a traditional Chinese medicine composition for treating inflammatory bowel disease as well as a preparation method and application thereof, and belongs to the technical field of medicines. The traditional Chinese medicine composition is prepared from the following components in parts by mass: 15-17 parts of radix pulsatillae, 10-12 parts of cortex fraxini, 10-12 parts of wine-processed rhizoma coptidis, 30-32 parts of cortex phellodendri, 15-17 parts of radix paeoniae alba, 10-12 parts of radix angelicae sinensis, 10-12 parts of radix aucklandiae and 10-12 parts of liquorice root. The traditional Chinese medicine composition provided by the invention is prepared from natural medicines, has low side effects, and provides a new choice for rehabilitation treatment and prevention of patients with inflammatory bowel diseases.

The invention discloses a brain-targeted nasal-spray amphotericin B phospholipid complex and a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations, the brain-targeted nasal-spray amphotericin B phospholipid complex is prepared by adopting a film dispersion method, and the preparation method comprises the following steps: dissolving 15-hydroxystearic acid polyethylene glycol ester, phospholipid, cholesterol, amphotericin B and optional other auxiliary components in a solvent, removing the solvent until a film is formed, and drying to obtain the brain-targeted nasal-spray amphotericin B phospholipid complex. And carrying out hydration dispersion to obtain the amphotericin B-loaded phospholipid complex. According to the amphotericin B sodium deoxycholate injection, the problems that the traditional amphotericin B sodium deoxycholate injection is high in renal toxicity, the intrathecal injection is poor in solubility, and low in bioavailability and patient compliance, large in side effect and the like due to the fact that the traditional amphotericin B sodium deoxycholate injection is difficult to penetrate through a blood brain After nasal administration, the drug is quickly delivered into the brain, so that the slow release of the drug is realized, the intracerebral bioavailability of the drug is improved, high brain targeting and low systemic toxic and side effects are realized, and good clinical application value and market prospect are achieved.

The invention provides an amoxicillin preparation and a preparation method thereof, and the preparation method comprises the following steps: preparing a temperature-sensitive polymer solution, uniformly mixing amoxicillin powder with chitosan and pretreated lactose, adding the mixture into the temperature-sensitive polymer solution, and carrying out spray drying to form amoxicillin-polymer composite particles, and carrying out multi-layer temperature sensitive coating treatment and curing. According to the invention, by using the temperature-sensitive polymer PNIPAM, the drug can be quickly released at an inflammation part under a high-temperature condition, the drug effect is improved, and the side effect is reduced. Due to the addition of the chitosan and the pretreated lactose, the solubility and bioavailability of the amoxicillin are improved, and the uniform distribution and sustained release of the medicine are ensured. The use of the plasticizer glycerol enhances the flexibility and stability of the polymer, and through curing treatment, the stability of the coating layer and the controllability of drug release are improved. The amoxicillin preparation disclosed by the invention has remarkable advantages in the aspects of improving the curative effect, reducing the side effect and improving the compliance of a patient.

This invention discloses a nystatin microsphere with targeted enhanced antifungal function, its preparation method, and its application. The microsphere uses sodium alginate as a carrier, internally encapsulating the antifungal drug nystatin. The surface is covalently modified with the β-glucan binding domain of the Dectin-1 protein, constructing a smart drug delivery system with fungal targeting function. The microsphere preparation process is simple and reproducible, and can be scalable using an emulsion-ionic crosslinking method combined with protein coupling technology. In vitro characterization shows that the microspheres have uniform particle size and stable dispersion, and Dectin-1 modification significantly enhances their specific binding ability against Candida albicans. This targeted delivery system, while successfully preserving drug activity, significantly improves the antifungal efficiency of nystatin through Dectin-1-mediated targeting, achieving efficacy close to that of free drug, and providing a new strategy for constructing highly efficient and long-acting antifungal agents.

This invention discloses a targeted, temperature-sensitive drug-loaded composite microsphere based on attapulgite, comprising primary drug-loaded composite microspheres and lauric acid. The primary drug-loaded composite microspheres include purified attapulgite, gypenosides, inulin, and folic acid. Gynostemma pentaphyllum saponins, inulin, and folic acid are adsorbed onto a mesoporous structure composed of purified attapulgite rod crystals. The surface rigid structure of the primary drug-loaded composite microspheres includes a large number of interlaced channels. Lauric acid is encapsulated within the surface rigid structure of the primary drug-loaded composite microspheres. The mass percentages of purified attapulgite, gypenosides, inulin, and folic acid are: 50-85 parts: 10-30 parts: 10-25 parts: 0.1-1 parts; the mass ratio of the primary drug-loaded composite microspheres to lauric acid is 1:2 to 1:3. This application not only enables temperature-controlled "on-off" drug release, significantly improving drug targeting and therapeutic precision, but also reduces the systemic toxicity of chemotherapy at its source, achieving highly efficient and low-toxicity synergistic therapy.

The invention discloses an ultrasonic labeling guided targeting nano liquid drop. The nano liquid drop comprises an inner core and a polymer layer coating the surface of the inner core, the inner core is perfluorinated carbon; the polymer layer comprises fluorine-containing polycaprolactone, a copolymer as shown in a formula I, an ultrasonic activation prodrug and a sound-sensitive agent; the perfluorinated carbon can be dissolved by the fluorine-containing polycaprolactone. According to the application, the tumor tissue is precisely treated by utilizing ultrasound to induce the tumor tissue to highly express the heat shock protein, so that the nano liquid drops modified with the heat shock protein targeting polypeptide are efficiently enriched at the tumor part, and the difference between the drug concentration in the tumor tissue and the drug concentration in other normal tissues is remarkably increased; the drug targeting selectivity and the drug release accuracy are improved.

The invention discloses application of a novel bone targeted drug delivery system based on specific bisphosphonate in new drug development and clinical application. The invention relates to an osteogenesis targeted drug conjugate, which is characterized in that the osteogenesis targeted drug conjugate BP-Btz is prepared by combining bisphosphonate (BP) without anti-bone resorption activity with a proteasome inhibitor bortezomib (Btz). The conjugate realizes local release of Btz in a bone microenvironment through the bone targeting ability of BP, the Btz level in non-bone tissues is very low, the curative effect is improved, and systemic side effects are reduced. In-vitro research shows that BP-Btz has similar effects to Btz in the aspects of inhibiting osteoclast formation, reducing bone resorption and stimulating osteoblast differentiation. In-vivo research shows that BP-Btz is more effective than Btz in the aspect of increasing bone volume, and side effects are reduced at the same time. In the aspect of pharmacodynamics, BP-Btz can be combined with a bone matrix and release Btz under the condition that the pH is 4-5, so that the Btz concentration in bone is higher, the half-life period is longer, and the drug resistance of Btz is effectively overcome. Therefore, the bone targeted drug delivery system can provide a new method for innovative application of drugs, and has important clinical application prospects and commercial potential.

This invention discloses a sonodynamic synergistic thrombolysis system and its application. The system includes a tissue plasminogen activator variant, a sonosensitive agent, and an ultrasound source. The tissue plasminogen activator variant is an intravenously administered formulation, the sonosensitive agent is an intravenously infused formulation, and the ultrasound source is used to emit ultrasound during sonosensitive agent administration to activate the agent. This invention significantly improves thrombolysis efficiency and reduces thrombolytic agent dosage and bleeding risk through the dual synergistic effect of TNK-tPA enzymatic hydrolysis and sonodynamic chemical oxidation. The system can significantly improve vascular recanalization rate and blood flow velocity recovery rate, and has high biocompatibility. This invention is applicable to thrombolytic treatment of various thrombotic diseases and has the advantages of simple operation, strong targeting, and wide application range.

The invention provides a rectal administration device which is used for solving the problem that the treatment effect is affected by poor absorption or non-uniform distribution of medicine in the digestive tract in the intestinal disease treatment mode in the prior art. The dosing device comprises a shell, a plurality of pumping mechanisms are fixed to the shell, each pumping mechanism comprises a fixing frame, a fixing groove is formed in the front end of the fixing frame and can contain an output pipe, a liquid outlet is formed in one end of the output pipe, a push plate is arranged in the output pipe in a sealed sliding mode, a push rod penetrating through the output pipe is fixed to the push plate, and a telescopic transmission mechanism is arranged in the fixing frame. An output shaft of the telescopic transmission mechanism drives the push rod through a push rod fixator, the fixing groove is provided with an output pipe fixator, the liquid outlet is connected with an infusion catheter, and a plurality of side holes are arrayed in the side wall of the end, away from the liquid outlet, of the infusion catheter. The device is convenient to carry, operate and use, the treatment flexibility is improved, meanwhile, part of components such as the medicine pushing device can be repeatedly used, the medical cost is reduced, and generation of medical waste is reduced.

The invention discloses a parabacteroides coumarini vesicle nano preparation for PD-L1 targeted synergistic chemotherapy as well as preparation and application of the parabacteroides coumarini vesicle nano preparation. The nano preparation takes a parabacteroides coumarini-sourced membrane vesicle as a carrier, a chemical drug apatinib is loaded in the nano preparation, the surface of the nano preparation is modified with an anti-PD-L1 antibody through chemical coupling, and the nano preparation is named as Apatinib-MVsaPD-L1; according to the nano preparation, apatinib and a PD-L1 antibody can be synergistically delivered to a breast cancer focus, so that the synergistic interaction of chemotherapy and immune checkpoint blocking is realized; in-vitro experiments show that the nano preparation can significantly inhibit proliferation of breast cancer cells and induce apoptosis of the breast cancer cells; in-vivo experiments show that the compound can effectively inhibit tumor growth and remarkably increase infiltration of CD8 < + > T cells and TNF-alpha < + > CD8 < + > T cells in a tumor microenvironment, has no toxic or side effect, and provides a new safe and efficient drug delivery platform for combined treatment of breast cancer.

The invention provides a tumor microenvironment response pharmaceutical composition as well as a preparation method and application thereof. The tumor microenvironment response pharmaceutical composition comprises a pH-sensitive amphiphilic prodrug and a stabilizer, wherein the pH-sensitive amphiphilic prodrug is formed by condensing a small molecular chemical drug and an auxiliary molecule; the stabilizer comprises lipid and cholesterol, the lipid is non-ionizable neutral lipid, and the phase change temperature range is-20 to 80 DEG C. The drug release is accurate, the targeting property is strong, the stability of the drug in vivo is high, systematic toxic and side effects are reduced, the in-vivo circulation time of the drug is prolonged, and the drug loading efficiency (gt; 70%) and treatment effect. The medicine is suitable for treating various cancers such as breast cancer, lung cancer and prostatic cancer.

This invention relates to the field of biopharmaceutical technology, and in particular to an antibody-targeted modified dual-strain prebiotic delivery system, its preparation method, and its applications. This invention modifies VCAM-1 antibody fragments onto *AKK* bacteria and *Bifidobacterium lactis* Probio-M8, then utilizes fructooligosaccharides and inulin as prebiotics to enhance probiotic metabolism and promote intestinal colonization. Finally, it coats the system with hydroxypropyl methylcellulose phthalate (HPMCP) enteric coating to construct the antibody-targeted modified dual-strain prebiotic delivery system—V-PM8-Am-FI-HPMC. The V-PM8-Am-FI-HPMC provided by this invention can simultaneously achieve intestinal flora regulation, lipid metabolism balance, inflammation suppression, ischemia improvement, and vascular anti-calcification, ultimately achieving the purpose of treating and / or improving atherosclerosis, while ensuring targeting and safety.

The invention discloses a replicative oncolytic adenovirus capable of blocking a TNF-TNFR2 signal channel as well as a preparation method and application of the replicative oncolytic adenovirus. The invention relates to a replicating oncolytic adenovirus for blocking a TNF-TNFR2 signal channel. The replicating oncolytic adenovirus for blocking the TNF-TNFR2 signal channel comprises a coding gene nucleotide sequence of a TNF antagonist, a TNFR2 antagonist or a combined molecule of the TNFR2 antagonist and a CD47 antagonist. The invention also discloses the application of the replicative oncolytic adenovirus for blocking the TNF-TNFR2 signal channel in preparation of anti-tumor drugs. According to the invention, by blocking a TNF-TNFR2 signal channel and utilizing the replicative oncolytic adenovirus to specifically replicate and dissolve cells in tumor cells, the pertinence and effectiveness of tumor treatment are enhanced.

The invention provides a construction method of a fatty acid modified chitosan oligosaccharide derivative, a preparation method of cationic nano-micelles and application of the cationic nano-micelles in lipid droplet degradation and targeted obesity therapy by combining photothermal therapy. By covalently modifying fatty acid on a chitosan oligosaccharide skeleton, the cationic micelle capable of entrapping small molecule drugs and targeting adipose tissues is obtained. The compound is combined with medicines such as a photo-thermal agent or a browning agent for use, can be used for targeted therapy of obesity after being loaded on a microneedle, and can effectively reduce lipid accumulation of adipose tissues and regulate whole body metabolism.

The invention relates to the technical field of intestinal tract treatment, and discloses an edged capsule movement complete ileum hovering device and method, which comprises a peristaltic shell, a driving mechanism is arranged at the tail end of the peristaltic shell, a hovering mechanism is arranged in the peristaltic shell, an administration mechanism is arranged at the head end of the peristaltic shell, and a linkage mechanism is further arranged at the position, close to the administration mechanism, of the peristaltic shell; the driving mechanism is arranged in the wriggling shell, the driving mechanism drives an opposite lantern ring of the hovering mechanism to move oppositely, so that a connecting rod assembly drives a movable assembly to form an opening state, the device hovers at the ileum section, and a linkage mechanism drives the dosing mechanism to form a wriggling state along with the intestinal tract and a hovering continuous dosing state; a patient with the ileitis disease can obtain more accurate and effective treatment, the medicine directly acts on a focus area, and the risk of systemic absorption and adverse reaction is reduced; meanwhile, the continuous administration mode ensures that the effective drug concentration is maintained at the focus part for a long time, and inflammation fading and tissue repairing are facilitated.